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The development and SAR of pyrrolidine carboxamide 11β-HSD1 inhibitors
- Source :
-
Bioorganic & Medicinal Chemistry Letters . May2010, Vol. 20 Issue 9, p2897-2902. 6p. - Publication Year :
- 2010
-
Abstract
- Abstract: The design and development of a series of highly selective pyrrolidine carboxamide 11β-HSD1 inhibitors are described. These compounds including PF-877423 demonstrated potent in vitro activity against both human and mouse 11β-HSD1 enzymes. In an in vivo assay, PF-877423 inhibited the conversion of cortisone to cortisol. Structure guided optimization effort yielded potent and stable 11β-HSD1 selective inhibitor 42. [Copyright &y& Elsevier]
- Subjects :
- *PYRROLIDINE
*ENZYME inhibitors
*CORTISONE
*ENZYME activation
*DIABETES
Subjects
Details
- Language :
- English
- ISSN :
- 0960894X
- Volume :
- 20
- Issue :
- 9
- Database :
- Academic Search Index
- Journal :
- Bioorganic & Medicinal Chemistry Letters
- Publication Type :
- Academic Journal
- Accession number :
- 49817550
- Full Text :
- https://doi.org/10.1016/j.bmcl.2010.03.032